Composition for viral hepatitis c therapy

FIELD: medicine.

SUBSTANCE: invention can be used to treat an infection caused by the hepatitis C virus (HCV). A composition for HCV infection treatment of by the RNAi mechanism consists of complexes of lipopeptides of the OrnGlu (C16H33)2 composition, serving as a carrier, and siRNA molecules represented by 5'-AAAUCUCCAGGCAUUGAGCtt-3' (SEQ ID NO 1). Composition application on a transplantable cell culture of human hepatoma Huh-7, expressing the subgenomic replicon of HCV, causes a significant decrease in viral replicon expression by 20%.

EFFECT: high bioavailability with subcutaneous administration of the composition.

2 cl, 8 dwg, 4 tbl, 5 ex

 



 

Same patents:

FIELD: medicine.

SUBSTANCE: claimed invention relates to the field of veterinary and is intended for fighting porcine reproductive and respiratory syndrome (PRRS). The method includes the vaccination of pigs with PRRS with the provision of a reduction of hyperthermia duration and protection of lung integrity. The vaccine is obtained by a method, including mixing a live vaccine, prepared for immediate introduction, with an adjuvant-diluent (AD). The said adjuvant-diluent represents an "oil-in water" type emulsion, which contains per 100% of its weight: from 99 to 50 wt % of water and from 1 to 50 wt % of an oil adjuvant. The oil adjuvant contains per 100 % of its weight: from 1 to 95 wt % of at least one mineral oil and from 1 to 80 wt % of at least one SAS. The mineral oil represents oil of a Marcol or Draekol type. SAS represents an ester, obtained by the condensation of a fatty acid with sorbitol or mannitol.

EFFECT: obtaining the preparation for fighting reproductive and respiratory syndrome.

7 cl, 9 tbl, 1 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to a novel (2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate of general formula I or a stereoisomer or a pharmaceutically acceptable salt thereof, having properties of nucleoside inihibitors of RNA polymerase NS5B of the hepatitis C virus. The invention also relates to a method of producing compounds, pharmaceutical compositions and a medicinal agent based on said compounds. In general formula 1 , R1 is hydrogen, (CH3)2[(CH3)3C]Si, C2-C6acyl, optionally substituted with a benzyloxy group, NR5R6 group, wherein R5 and R6 are independently hydrogen or C1-C4alkyl; 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl or piperidin-4-ylcarbonyl; R2 and R3 are F or R2 is F or OH and R3 is CH3; R4 is hydrogen or methyl; Ar is phenyl, pyridyl or naphthyl, where the phenyl, pyridyl or naphthyl is optionally substituted with at least one of C1-3alkyl, C2-4alkenyl, C2-4alkynyl, C1-3alkoxy, F, Cl, Br, I, nitro, cyano, -N(C1-3alkyl)2; Pm is 2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl or 4-(4-amino-2-oxo-2H-pyrimidin-1-yl), wherein the amino group is optionally substituted with 1-pyrrol-2-ylcarbonyl, piperidin-3-ylcarbonyl, piperidin-4-ylcarbonyl or a C(O)R8 radical, where R8 is C1-C4alkyl, optionally substituted with a NR6R7 group, where R6 and R7 are independently hydrogen or C1-C4alkyl; C1-3alkoxy, optionally substituted with a phenyl; X is O or N-R9, where R9 is C1-C4alkyl, optionally substituted with OH or OCH3; n=1, 2 or 3.

EFFECT: compounds can be used to prevent and treat viral infections, including hepatitis C.

12 cl, 1 tbl, 11 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compounds intended for treatment of hepatitis C of formula

:

its stereoisomeric forms, pharmaceutically acceptable salts or solvates, where R1 represents hydrogen; R2 represents hydrogen, napthyl or phenyl, optionally substituted with 1, 2 or 3 substituents, selected from halogen and C1-C6alkyl; R3 and R4 represent hydrogen or C1-C6alkyl; R5 represents C1-C10alkyl, optionally substituted with C1-C6alkoxygroup, C3-C7cycloalkyl or benzyl; R8 represents hydrogen.

EFFECT: claimed are novel compounds and composition on their base, effective against hepatitis C.

12 cl, 4 ex, 1 tbl

Antiviral agent // 2546006

FIELD: medicine.

SUBSTANCE: antiviral agent of poly-N1-hydrazino(imino)methyl-1,6-hexane diamine-amino(imino)methyl-1,6-hexanediamine of general formula: wherein: HX is an acid, n=3-20, m=4-20, possessing an activity on simple and complex RNA- and DNA-containing viruses of humans, animals, plants, bacteria and fungi.

EFFECT: what is created is the broad-spectrum antiviral agent possessing the activity on viruses found both intra-, and extracellularly.

9 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to organic chemistry, namely to bis-benzimidazole derivatives of formula I and their optional stereoisomers, pharmaceutically acceptable salts and solvates, wherein R and R' are independently specified in -CR1R2R3, phenyl substituted by 1 substitute specified in halogen; and tetrahydrofuranyl, wherein R1 is specified in C1-4alkyl optionally substituted by methoxy, hydroxyl or dimethylamino; C3-6cycloalkyl; phenyl optionally substituted by 1, 2 or 3 substitutes optionally specified in halogen, C1-4alkoxy, trifluoromethoxy, or 2 substitutes on adjoining atoms of the ring form 1,3-dioxolane group; benzyl substituted by halogen or methoxy; pyridinyl; indolyl; pyridinylmethyl or indolylmethyl; R2 is specified in hydrogen, hydroxyl, di-C1-4alkylamino, (C3-6cycloalkyl) (C1-4alkyl)amino, C1-4alkylcarbonylamino, phenylamino, C1-4alkyloxycarbonylamino, (C1-4alkyloxycarbonyl)(C1-4alkyl)amino, C1-4alkylaminocarbonylamino, tetrahydro-2-oxo-1(2H)-pyrimidinyl, pyrrolidin-1-yl, piperidin-1-yl, 3,3-difluoropiperidin-1-yl, morpholin-1-yl, 7-azabicyclo[2.2.1]hept-7-yl and imidazol-1-yl; and R3 represents hydrogen or C1-4alkyl or CR2R3 together form carbonyl; or CR1R3 form cyclopropyl group. The invention also refers to a pharmaceutical composition based on a compound of formula I.

EFFECT: there are prepared bis-benzimidazole derivatives possessing the inhibitory activity on hepatitis C virus.

9 cl, 4 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: invention refers to biotechnology and immunology. There are described antibodies and their functional equivalents specifically binding to RSV. Also, the invention refers to nucleotide sequences coding the above antibody, as well as to the cells producing antibodies, and to methods for producing the above antibodies.

EFFECT: invention can be used in medicine.

23 cl, 4 dwg, 3 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to heterocyclic compounds of general formula I

or to pharmaceutically acceptable salts or solvates or stereoisomers thereof, where R and R* are each independently -CR1R2R3, C1-4alkylamino, benzylamino, C6-10arylamino, heteroC4-7cycloalkyl containing 1 heteroatom selected from O; where R1 is selected from C1-4alkyl; phenyl, optionally substituted with 1, 2 or 3 substitutes independently selected from halogen, C1-4alkyl, C1-4alkoxy, trifluoromethoxy or 2 substitutes at neighbouring ring atoms, which form a 1,3-dixolane group; benzyl, optionally substituted with a halogen or methoxy; phenylsulphonylmethyl; C3-5heteroaryl containing 1 to 2 heteroatoms independently selected from N and O; C3-5heteroarylmethyl containing 1 to 2 heteroatoms selected from N and C3-6cycloalkyl; R2 is selected from hydrogen, hydroxyl, di-C1-4alkylamino, C1-4alkylcarbonylamino, C1-4alkyloxycarbonylamino, C1-4alkylaminocarbonylamino, piperidin-1-yl or imidazol-1-yl; R3 is hydrogen or, alternatively, R2 and R3 together form an oxo group; or R1 and R3 together form cyclopropyl; under the condition that if one of R and R* is -CH(C6H5)N(CH3)2, the other cannot be -CH(C6H5)NHC(=O)OCH3; and if R and R* are identical, R1 is not phenyl, when R2 is hydroxyl, acetylamino, methoxycarbonylamino or tert-butoxycarbonylamino, and R3 is hydrogen; and R1 is not C1-4alkyl, when R2 is C1-4alkyloxycarbonylamino, and R3 is hydrogen. The invention also relates to a pharmaceutical composition based a compound of formula I and use thereof.

EFFECT: obtaining novel compounds which are useful in preventing or treating HCV infection.

9 cl, 2 tbl, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a sodium salt of formula I compound in the solid amorphous form. The sodium salt of formula (I) compound is obtained by (a) the preparation of a mixture of the formula I compound in a non-aqueous solvent and a water solution of sodium hydroxide; and (b) drying by spraying of the mixture (a) in a spray-drying device. The stage (a) includes mixing the sodium hydroxide solution with the said solvent and further addition of the formula I compound. The solvent is represented by halogen-containing hydrocarbon. The invention also relates to a pharmaceutical composition, possessing HCV inhibiting properties, including sodium salt of the formula I compound in the amorphous form, and a pharmaceutically acceptable carrier.

EFFECT: sodium salt of the formula (I) compound for application as HCV inhibitor and medication for HCV treatment.

10 cl, 7 dwg, 3 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel polyheterocyclic compounds of formulas Ia or Ib, given below, stereoisomers, pharmaceutically acceptable salts or their mixture, where m=0.1 or 2; n=0.1 or 2; p=0.1 or 2; q=0.1 or 2; r=0. 1, 2 or 3; stands for a single bond or a double bond; and stands for a double bond in a macrocyclic internal combination with cyclopropyl formyl; stands for a single bond in a cycle D, E, E1 and G, where D and G independently stand for oxygen, E and E1 independently stand for C(Ra)(Rb); R10 stands for hydrogen; Ra, Rb and Rc independently on each other stand for hydrogen; when r=0 E is absent, D and E1 are directly bound; L stands for methylene (CRbRc); T stands for nitrogen (N) or CH; U stands for carbon (C); W stands for oxygen; X stands for oxygen; Y stands for nitrogen (N) or CH; Z stands for OH; C1-C20 alkyl-sulphonylamido, C3-C20-cycloalkyl-sulphonylamido; R1 and R2 independently stand for C1-C20-alkyl, C3-C20 cycloalkyl, C6-C12 arylamine, C1-C20 alkoxycarbonyl-amino, C2-C20 heterocyclic sulphonylamide ring; R3, R4, R5, R6 - independently stand for H; R7, R8 and R9 independently stand for H. The compounds inhibit replication of protease NS3 of the hepatitis C virus.

EFFECT: improved properties of the compounds.

7 cl, 1 tbl, 11 dwg, 118 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, namely to pharmacology and virology, and deals with the creation of medications, possessing an anti-retroviral activity.

EFFECT: claimed is a pharmaceutical composition, containing an activated-potentiated form of antibodies to the HIV protein or peptide.

13 cl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to field of encapsulation, in particular to method of obtaining microcapsules of medications from cephalosporin group in human leukocyte interferon (β- or α-interferon) coat. In accordance to invention cephalosporin powder and E472c preparation are added to 1% water solution of human leukocyte interferon in α- or β-form and mixed until reaction mixture components dissolve. After formation of transparent solution butanol and acetone are added. Obtained suspension of microcapsules is filtered, washed and dried. Process of obtaining microcapsules is realised at 25°C for 15 min.

EFFECT: invention provides simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of their obtaining (increase of output by weight).

4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to the field of microencapsulation, in particular to a method of obtaining microcapsules of medications of a cephalosporin group. The method is characterised by the fact that human serum albumin is used as an envelope for microcapsules, with the addition to a water solution of albumin of a powder of a cephalosporin group preparation in the presence of a surface-active substance E472c, the ratio of quantity of the cephalosporin group preparation to albumin counted per dry substance constitutes from 1:1 to 3:1, the obtained mixture is mixed to the complete dissolution of components with the slow drop-by-drop addition of butanol as the first precipitating agent, and then acetone as the second precipitating agent, the obtained suspension of microcapsules is filtered, washed with acetone, dried in a dessicator, the process of obtaining microcapsules is realised at 25°C.

EFFECT: method provides the simplification and acceleration of the process of obtaining microcapsules of the water-soluble medications of a cephalosporin group in human serum albumin, and reduction of loss in obtaining the microcapsules.

3 ex

FIELD: medicine.

SUBSTANCE: method involves professional oral hygiene is carried out consisting in ultrasonic removal of supra- and subgingival dental deposits and polishing of supragingival teeth. Bite splinting and recovery of dentition integrity may be required. After dissecting a mucoperiosteal flap according to the known technique, an incision area is sanitated by means of a photodynamic therapy (PDT). The PDT is conducted with the use of a diode laser at wave length 660±5 nm and emitting power 0.5-1.0 Wt. The photosensitiser "Photoditasin" in the form of 0.5% gel is introduced by means of a cannula into dental gaps, under the dissected segments of the flap and onto the mucosal tissue for 5 minutes. The photosensitiser is washed out, and the gingival pockets are repeatedly exposed to laser light for 2-3 min in the same environment. Sterile osteoplastic material is introduced into bone defects, and the flap is sutured together.

EFFECT: effective cleansing of the surgical area, eliminating the periodontal inflammation, stimulating tissue osteogenesis and regeneration, stabilising the processes of bone tissue absorption of alveolar interdental septa and preserving the tissues.

2 cl, 1 ex

FIELD: chemistry.

SUBSTANCE: enzyme is coated with an internal envelope of a polycation and an external envelope of a polyanion, where the polycation used is protamine or polyarginine, the polyanion used is a block-copolymer of poly(glutamic acid) and polyethylene glycol, wherein the nanoparticle has a hydrodynamic diameter in the range of 40-70 nm. The invention also relates to a dispersion which contains nanoparticles of the antioxidant enzyme superoxide dismutase for medical use in the form of polyelectrolyte complexes of the type enzyme/polycation/polyanion, and a method of producing said dispersion.

EFFECT: high stability of the enzyme in a foreign medium with preservation of the activity of the enzyme.

9 cl, 1 dwg, 1 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of encapsulation, in particular to method of obtaining microcapsules Biopag-D in envelope of human leukocytic interferon (β- or α-interferon). According to invention method, suspension of Biopag-D in water is added to 1-% water solution of interferon in presence of medication E472c and mixed to transparent solution. Suspension of Biopag-D and interferon solution are taken in weight ratio 3:1 or 2.5:1. Butanol, and then acetone taken in ratio 1:5% vol/vol are added. Obtained suspension of microcapsules is filtered, washed and dried. Process of obtaining microcapsules is realised at 25°C for 15 min.

EFFECT: invention ensures simplification and acceleration of process of obtaining microcapsules, reduction of loss in the process of their obtaining (increase of output by weight).

3 ex

FIELD: medicine.

SUBSTANCE: group of inventions refers to medicine and concerns ear-drum or external auditory canal restoration. That is ensured by presented an agent containing a combination of gelatine sponge, basic fibroblast growth factor and fibrin glue, as well as using these ingredients for producing the agent. The method involves placing gelatine sponge containing a therapeutically effective amount of basic fibroblast growth factor within an ear-drum perforation or a defect of soft tissue of the external auditory canal and covering the sponge with fibrin glue.

EFFECT: inventions provide the effective defect closure and tissue restoration, including in the case where common methods are not applicable.

6 cl, 2 dwg, 3 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation, particularly to a method for cephalosporin microencapsulation. The method is characterised by the fact that a microcapsule coating is human serum albumin; an aqueous solution of albumin is added with the cephalosporin powder in the presence of a surfactant; the ratio of the cephalosporin preparation to albumin in terms of dry substance makes from 1:1 to 3:1; the prepared mixture is stirred and added with isopropanol as the first precipitation agent, and then acetone as the second precipitation agent; the prepared microcapsule suspension is filtered, washed in acetone, dried in a drying cabinet; the microencapsulation process is performed at 25°C.

EFFECT: method provides simplifying and fastening the microencapsulation process of water-soluble cephalosporins in serum albumin, reducing the loss accompanying the microencapsulation process.

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to microencapsulation, particularly to a method for cephalosporin microencapsulation. The method is characterised by the fact that a microcapsule coating is human serum albumin; a powder cephalosporin preparation is added to an aqueous solution in the presence of a surfactant; a ratio of the powder cephalosporin preparation to albumin at a dry substance matter makes 1:1 to 3:1; the prepared mixture is agitated, methylcarbinol is added as a first precipitator, and then isopropanol is added as a second precipitator; the prepared suspension of microcapsules is filtered, washed in isopropanol, dried in an exiccator; the process of microcapsules is performed at 25°C.

EFFECT: method provides simplifying and accelerating the process of microcapsules of water-soluble cephalosporin preparations in serum albumin, reducing the loss accompanying the process of microcapsules (higher weight yield).

3 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to bioencapsulation, particularly to a method for cephalosporin bioencapsulation, wherein a microcapsule coating is human leucocyte α- or β-interferon. According to the method, power cephalosporin 0.060 g or 0.075 g respectively and E472c preparation 0.05 g as a surfactant are added to 1% aqueous human leucocyte α- or β-interferon 2 g or 2.5 g; the prepared mixture is stirred until the ingredients of the reaction mixture are dissolved completely. Forming a transparent solution is followed by slow drop-by-drop addition of methyl carbinol 1 ml as a first precipitating agent and isopropanol 5 ml as a second precipitating agent; then acetone is added, and the mixture is dried. The method is implemented at 25°C with no special equipment applied.

EFFECT: simplifying and accelerating the process of microcapsules in interferon and higher weight yield.

4 ex

FIELD: biotechnologies.

SUBSTANCE: biologically active material, a matrix shaping agent and at least two glass-shaping agents are combined in a water solvent so that a viscous suspension is obtained. The obtained suspension is quickly frozen in liquid nitrogen with formation of solid frozen particles in the form of granules, drop particles or fibres. Frozen particles are degassed under vacuum gauge pressure of 0 to 2000 mTorr (266.6 Pa) and at the temperature below a composition freezing point during 1-30 minutes. Further, particles are subject to primary drying at the pressure of 2000 to 10000 mTorr (266.6 to 1333 Pa) and at the temperature above the particle freezing point. Secondary drying of particles is performed at full vacuum and temperature of 20°C to 70°C during the period of the time sufficient for reduction of activity of water of the obtained composition to Aw 0.3 or below.

EFFECT: excluding boiling or excess foaming of a composition at simultaneous achievement of considerable acceleration of drying and high allowable load of the composition.

11 cl, 9 dwg, 1 tbl, 16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions relates to medicine and deals with immunogenic composition, which contains combination of the following parts: (i) polymerase part, which contains at least 450 amino acid residues of polymerase protein, obtained from first HBV-virus; (ii) core part, which contains at least 100 amino acid residues of heart-shaped protein, obtained from second HBV-virus; and (iii) envelope part, which contains one or more immunogenic area from 20-100 successive amino acid residues of HBsAg protein, obtained from third HBV-virus; or combination of nucleic acid molecules, coding said polymerase part, said core part and said envelope part. Group of inventions also deals with nucleic acid molecule for stimulation or increase of immune response to HBV; vector for stimulation or increase of immune response to HBV, containing one or more nucleic acid molecule; infectious viral particle for stimulation or increase of immune response to HBV; method of treatment or prevention of HBV-infections or HBV-associated disease or pathological condition; set for application in treatment of HBV-infection.

EFFECT: group of inventions ensures stability and preservation of high immunogenicity of vectors, applied in composition.

51 cl, 7 dwg, 2 ex

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